The aim of this work was to develop, optimize and characterize a silymarin-laden polyvinylpyrrolidone (PVP)-polyethylene glycol (PEG) polymeric composite to resolve low aqueous solubility and dissolution rate problem of the drug. A number of silymarin-laden polymeric formulations were fabricated with different quantities of PVP K-30 and PEG 6000 by the solvent-evaporation method. The effect of PVP K-30 and PEG 6000 on the aqueous solubility and dissolution rate was investigated. The optimized formulation and its constituents were characterized using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) techniques. Both the PEG 6000 and PVP K-30 positively affected the aqueous solubility and dissolution rate of the drug. In particular, a formulation consisting of silymarin, PVP K-30 and PEG 6000 (0.25/1.5/1.5, w/w/w) furnished the highest solubility (24.39±2.95 mg/mL) and an excellent dissolution profile (~100% in 40 min). The solubility enhancement with this formulation was ~1150-fold as compared to plain silymarin powder. Moreover, all the constituents existed in the amorphous state in this silymarin-laden PVP-PEG polymeric composite. Accordingly, this formulation might be a promising tool to administer silymarin with an enhanced effect via the oral route.

To develop a novel revaprazan-loaded gelatin microsphere with enhanced solubility and oral bioavailability, numerous gelatin microspheres were prepared using a spray-drying technique. The impact of gelatin amount on drug solubility in the gelatin microspheres was investigated. The physicochemical properties of the selected gelatin microsphere, such as shape, particle size and crystallinity, were evaluated. Moreover, its dissolution and pharmacokinetics in rats were assessed in comparison with revaprazan powder. Amongst the gelatin microspheres tested, the gelatin microsphere consisting of revaprazan and gelatin (1:2, w/w), which gave about 150-fold increased solubility, had the most enhanced drug solubility. It provided a spherical shape, amorphous drug and reduced particle size. Furthermore, it gave a higher dissolution rate and plasma concentration than did revaprazan powder. Particularly, it gave about 2.3-fold improved oral bioavailability in comparison with revaprazan powder. Therefore, this novel gelatin microsphere system is recommended as an oral pharmaceutical product of poorly water-soluble revaprazan.

Background/Objective: Periodontitis is a widely spread oral infection and various antibiotics are utilized for its treatment, but high oral doses and development of antibiotic resistance limit their use. This study was aimed at development of natural polymer-based mucoadhesive bilayer films loaded with moxifloxacin hydrochloride (Mox) and clove essential oil (CEO) to potentially combat bacterial infection associated with periodontitis. Methods: Films were synthesized by double solvent casting technique having an antibiotic in the gellan gum-based primary layer with clove oil in a hydroxyethyl cellulose-based secondary layer. Results: Prepared films were transparent, flexible, and showed high antibacterial response against both gram-positive and gram-negative bacteria. The films showed excellent pharmaceutical attributes in terms of drug content, folding endurance, swelling index, and mucoadhesive strength. Solid state characterization of formulation showed successful incorporation of drug and oil in separate layers of hydrogel structure. An in-vitro release study showed an initial burst release of drug followed by sustained release for up to 48 hours. Conclusion: The prepared mucoadhesive bilayer buccal films could be used as a potential therapeutic option for the management of periodontitis.